Nonsteroid Estrogen Antagonists

Its a nonsteroidal estrogen antagonist, which acts by preventing implantation due to embryouterine asynchrony, accelerated tubal transport and suppression of decidualization. It has no effect on pituitary or ovarian functions. It is taken 30 mg twice weekly for 12 weeks followed by once a week as long as fertility is to be suppressed. 

Lerner LJ, Holthaus JF, Thompson CR. A nonsteroidal estrogen antagonist 1-(p-2-diethylaminoethoxyphenyl)-1-phenyl-2-p-methoxyphenylethanol. Endocrinology 1958 63 295-318. 

CHEMICAL CONNECTIONS 19A Snake Venom Phospholipases 19B Nonsteroidal Estrogen Antagonists... 

Following is a synthesis for toremifene, a nonsteroidal estrogen antagonist whose structure is closely related to that of tamoxifen. 

In 2009, Snyder s group reported the first asymmetric total synthesis of ( )-napyradiomycin A1 93, a nonsteroidal estrogen antagonist isolated from Streptomyces bacteria... 

Ke HZ, Paralkar VM, Grasser WA, Crawford DT, Qi H, Simmons H, et al. (1998) Effects of CP-336,156, a new, nonsteroidal estrogen agonist/antagonist, on bone, serum cholesterol, uterus, and body composition in rat models. Endocrinology 139 2068-2076... 

Tamoxifen, a first-generation SERM, is a nonsteroidal triphenylethylene derivate routinely used in clinical practice for the treatment and prevention of breast cancer in high-risk populations (Robertson 2004). This drug produces an estrogen antagonist effect on the breast and an estrogen agonist effect... 

Raloxifene hydrochloride is a synthetic nonsteroidal drug derived from the benzothiophene and afferent to SERMs. It is known that raloxifene acts on metabolism, the skeleton, and the cardiovascular system as an estrogenic agonist (Khovidhunkit et al. 1999 Ettinger et al. 1999 Walsh et al. 1998), whereas it shows an estrogenic antagonist effect on reproductive organs such as the... 

Lasofoxifene is a new potent nonsteroidal SERM that binds with high affinity to ERs acting as a tissue-selective estrogen antagonist or agonist (Maeda et al. 2004). 

Nonsteroidal estrogen receptor antagonist competitively binds to estrogen receptors on estrogen-dependent breast cells... 

Rosati, R.L. and Da Silva, J.P. (1998) Discovery and predinical pharmacology of a novel, potent, nonsteroidal estrogen receptor agonist/antagonist, CP-336156, a diaryltetrahydronaphfhalene. Journal of Medicinal Chemistry, 41, 2928—2931. 

Evista Keoxifene hydrochloride LY 156758 Raloxifene hydrochloride. Nonsteroidal estrogen receptor mixed agonist-antagonist. Antiestrogen used to treat osteo-porosis. Solid mp = 258° km = 286 nm (c 32800 EtOH). Eli Ully 4 Co. 

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